Wu Liang, Tang Yuping, Shan Chenxiao, Chai Chuan, Zhou Zhu, Shi Xuqin, Ding Ning, Wang Jiaying, Lin Liping, Tan Renxiang
State Key Laboratory Cultivation Base for TCM Quality and Efficacy, Nanjing University of Chinese Medicine, Nanjing, 210023, China.
Center for Drug Safety Evaluation and Research, School of Medicine and Life Sciences, Nanjing University of Chinese Medicine, Nanjing, 210023, China.
J Mass Spectrom. 2018 Feb;53(2):99-108. doi: 10.1002/jms.4041.
As the most important marker component in Carthamus tinctorius L., hydroxysafflor yellow A (HSYA) was widely used in the prevention and treatment of cardiovascular diseases, due to its effect of improving blood supply, suppressing oxidative stress, and protecting against ischemia/reperfusion. In this paper, both an in vitro microsomal incubation and an in vivo animal experiment were conducted, along with an LC-Q-TOF/MS instrument and a 3-step protocol, to further explore the metabolism of HSYA. As a result, a total of 10 metabolites were searched and tentatively identified in plasma, urine, and feces after intravenous administration of HSYA to male rats, although no obvious biotransformation was found in the simulated rat liver microsomal system. The metabolites detected involving both phase I and phase II metabolism including dehydration, deglycosylation, methylation, and glucuronic acid conjugation. A few of the metabolites underwent more than one-step metabolic reactions, and some have not been reported before. The study would contribute to a further understanding of the metabolism of HSYA and provide scientific evidence for its pharmacodynamic mechanism research and clinical use.
作为红花中最重要的标志性成分，羟基红花黄色素A（HSYA）因其具有改善血液供应、抑制氧化应激以及抗缺血/再灌注的作用，而被广泛应用于心血管疾病的防治。本文采用体外微粒体孵育和体内动物实验，并借助LC-Q-TOF/MS仪器及三步流程，进一步探究HSYA的代谢情况。结果显示，给雄性大鼠静脉注射HSYA后，在血浆、尿液和粪便中总共搜索并初步鉴定出10种代谢产物，尽管在模拟大鼠肝微粒体系统中未发现明显的生物转化现象。检测到的代谢产物涉及I相和II相代谢，包括脱水、去糖基化、甲基化和葡萄糖醛酸结合。部分代谢产物经历了不止一步的代谢反应，且其中一些此前未见报道。该研究将有助于进一步了解HSYA的代谢情况，并为其药效学机制研究和临床应用提供科学依据。
